Drug intelligence / Profile preview

INCB053914

Development stage
Discontinued
Lead developer
Incyte
Modality
Small Molecules
Administration
Oral
01

Overview

INCB053914 is a novel, ATP-competitive, small-molecule pan-inhibitor of the PIM (Proviral Integration site for Moloney murine leukemia virus) serine/threonine kinases, specifically targeting the PIM1, PIM2, and PIM3 isozymes. Developed by Incyte Corporation, the drug was designed to inhibit the PIM kinase family, which is frequently overexpressed in hematologic and solid tumors and plays a critical role in promoting cell survival, proliferation, and resistance to apoptosis through the regulation of various signaling pathways, including the MYC and mTOR pathways. INCB053914 was evaluated in Phase 1/2 clinical trials for advanced hematologic malignancies, such as acute leukemia, myelodysplastic syndromes, and myelofibrosis, as well as in combination with the PI3Kδ inhibitor parsaclisib for relapsed or refractory diffuse large B-cell lymphoma (DLBCL). However, Incyte has since discontinued the clinical development of the compound.

Other names
uzansertib
02

Targets

PIM1 (Proviral integration site for moloney murine leukemia virus kinase 1)PIM2 (Proto-oncogene serine/threonine-protein kinase Pim2)PIM3 (Proviral integration site for Moloney murine leukemia virus kinase 3)

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